Berberine-baicalin compound and preparation method and application thereof

A technology of diglucoside and baicalin, which is applied in the preparation of sugar derivatives, chemical instruments and methods, and pharmaceutical formulations, to achieve the effects of enhancing drug efficacy, facilitating large-scale industrial production, and meeting various needs

Inactive Publication Date: 2016-05-04
PI & PI BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there are no public or related reports on the patents and related research on the chemical synthesis of berberine and baicalin into new multinuclear molecules

Method used

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  • Berberine-baicalin compound and preparation method and application thereof
  • Berberine-baicalin compound and preparation method and application thereof
  • Berberine-baicalin compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] (1a) Synthesis of berberine derivatives: Weigh 1 part by weight of berberine, add 150 (150-200) parts by weight of acetonitrile, heat to boiling at 85°C, add X(CH 2 ) n Y40 (20-40) parts by weight, reflux for 3 hours, concentrate the reaction solution to 50 (50-100) parts by weight, cool and crystallize, filter, wash the crystals with an appropriate amount of acetonitrile, combine the washing liquid with the filtrate, and recover the acetonitrile . The filter residue was dissolved in 30 parts by weight of methanol, cooled to crystallize, filtered, washed with methanol, and combined with the above crystals to obtain a berberine derivative with a calculated yield of 56.34%. Among them, X(CH in this embodiment 2 ) n Y, X, and Y are all Br, n=4, and the gained berberine derivative is berberine-9-oxobutyl bromide, and its 1 HNMR picture as shown figure 1 as shown, 13 CNMR picture as figure 2 shown. in, figure 1 The attribution of H in is shown in Table 1, figure ...

Embodiment 2

[0091] In addition to the amount of acetonitrile, X(CH 2 ) n Except that the amount of Y and the concentration of the reaction solution are different, the preparation method of dixanthoside in this implementation is basically the same as that in Example 1. Among them, the X(CH of the present embodiment 2 ) n Y, X, Y are all Cl, n=5.

Embodiment 3

[0093] In addition to the amount of acetonitrile, X(CH 2 ) n Except that the amount of Y and the concentration of the reaction solution are different, the preparation method of dixanthoside in this implementation is basically the same as that in Example 1. Among them, the X(CH of the present embodiment 2 ) n Y, X and Y are all S, n=6.

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Abstract

The invention discloses a berberine-baicalin compound which has the structure shown as a general formula (I), and further discloses a preparation method of the compound and application of the compound in preparation of a drug for treating ulcerative enteritis. The compound is prepared by synthesizing berberine and baicalin. Compared with berberine and baicalin, the compound has the advantages that the toxicity of the multi-core molecular compound is significantly reduced, absorption is significantly improved, the bioavailability is improved, the metabolism time is prolonged, the long-acting effect can be achieved, and the medical efficacy of resisting the ulcerative enteritis and pathogenic bacteria is enhanced.

Description

technical field [0001] The invention relates to the fields of medicinal chemistry and pharmacotherapeutics, in particular to a dixanthoside, a preparation method of the compound and an application in preparation of medicines for treating ulcerative enteritis. Background technique [0002] Ulcerative colitis (UC), also known as chronic nonspecific ulcerative colitis or idiopathic ulcerative colitis, is a common chronic intestinal disease. heterosexual inflammation. The lesions are mainly in the mucosa and submucosa of the colon, showing continuous and diffuse distribution, most of which involve the rectum and sigmoid colon. The main clinical manifestations are abdominal pain, diarrhea, mucus pus and blood in the stool, tenesmus, etc. Some patients have extraintestinal manifestations, such as joint, liver and bile duct diseases, and eye and skin damage; Between 20 and 50 years old, but no significant sex difference. Epidemiological statistics at home and abroad show that th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07C07H1/00A61K31/706A61P1/04
CPCC07H17/07C07H1/00
Inventor 李卫民袁晓荣向路周东斌
Owner PI & PI BIOTECH
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